PH12017501326A1 - Tgf-� inhibitors - Google Patents

Tgf-� inhibitors

Info

Publication number
PH12017501326A1
PH12017501326A1 PH12017501326A PH12017501326A PH12017501326A1 PH 12017501326 A1 PH12017501326 A1 PH 12017501326A1 PH 12017501326 A PH12017501326 A PH 12017501326A PH 12017501326 A PH12017501326 A PH 12017501326A PH 12017501326 A1 PH12017501326 A1 PH 12017501326A1
Authority
PH
Philippines
Prior art keywords
tgf
inhibitors
compound
disclosed
prodrugs
Prior art date
Application number
PH12017501326A
Inventor
Todd Kinsella
Marina Gelman
Hui Hong
Ihab S Darwish
Rajinder Singh
Jiaxin Yu
Robert M Borzilleri
Upender Velaparthi
Peiying Liu
Chetan Darne
Hasibur Rahaman
Jayakumar Sankara Warrier
Original Assignee
Rigel Pharmaceuticals Inc
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Rigel Pharmaceuticals Inc, Bristol Myers Squibb Co filed Critical Rigel Pharmaceuticals Inc
Publication of PH12017501326A1 publication Critical patent/PH12017501326A1/en

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R' are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-B, and can be used to treat disease by blocking TGF-B signaling.
PH12017501326A 2015-03-02 2017-07-21 Tgf-� inhibitors PH12017501326A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562127109P 2015-03-02 2015-03-02
PCT/US2016/019830 WO2016140884A1 (en) 2015-03-02 2016-02-26 TGF-β INHIBITORS

Publications (1)

Publication Number Publication Date
PH12017501326A1 true PH12017501326A1 (en) 2017-12-18

Family

ID=55543068

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12017501326A PH12017501326A1 (en) 2015-03-02 2017-07-21 Tgf-� inhibitors

Country Status (24)

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US (3) US9884868B2 (en)
EP (1) EP3265454B1 (en)
JP (1) JP6836998B2 (en)
KR (1) KR20170122799A (en)
CN (1) CN107406412B (en)
AR (1) AR103828A1 (en)
AU (1) AU2016226468B2 (en)
BR (1) BR112017017135A2 (en)
CA (1) CA2973602A1 (en)
CL (1) CL2017002207A1 (en)
CO (1) CO2017009891A2 (en)
EA (1) EA037112B1 (en)
ES (1) ES2789331T3 (en)
HK (1) HK1244785A1 (en)
IL (1) IL254187A0 (en)
MX (1) MX371167B (en)
MY (1) MY186133A (en)
PE (1) PE20171789A1 (en)
PH (1) PH12017501326A1 (en)
SG (1) SG11201705821XA (en)
TN (1) TN2017000374A1 (en)
TW (1) TW201639827A (en)
WO (1) WO2016140884A1 (en)
ZA (1) ZA201705527B (en)

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